Adamantyl Analogues of Paracetamol as Potent Analgesic Drugs via Inhibition of TRPA1

Paracetamol also known as acetaminophen, is a widely used analgesic and antipyretic agent. We report the synthesis and biological evaluation of adamantyl analogues of paracetamol with important analgesic properties. The mechanism of nociception of compound 6a/b, an analog of paracetamol, is not exerted through direct interaction with cannabinoid receptors, nor by inhibiting COX. It behaves as an interesting selective TRPA1 channel antagonist, which may be responsible for its analgesic properties, whereas it has no effect on the TRPM8 nor TRPV1 channels. The possibility of replacing a phenyl ring by an adamantyl ring opens new avenues in other fields of medicinal chemistry.

• Publication year

  2014

• Venue

  PLoS ONE

• Publication date

  2014-12-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1371/journal.pone.0113841PMID 25438056PMCID 4249970
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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